Omipalisib(GSK-458)

    • 货号:MC0349
      • CasNo:
      • 1086062-66-9
      • 分子式:
      • C25H17F2N5O3S
      • 纯度:
      • >98%
      • 靶点:
      • PI3K
      • IC50:
      • Ki: 0.019 nM (p110α), 0.13 nM (p110β), 0.024 nM (p110δ), 0.06 nM (p110γ), 0.18 nM (mTORC1), 0.3 nM (mTORC2)
      • 体外研究:
      • GSK2126458 potently inhibits the activity of common activating mutants of p110α (E542K, E545K, and H1047R) found in human cancer with Ki of 8 pM, 8 pM and 9 pM, respectively. GSK2126458 causes a significant reduction in the levels of pAkt-S473 with remarkable potency in T47D and BT474 cells with IC50 of 0.41 nM and 0.18 nM, respectively. Furthermore, GSK2126458 leads to a G1 cell cycle arrest and produces the inhibitory effect on cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines with IC50 of 3 nM and 2.4 nM, respectively[1]. The combination of GSK2118436 or GSK1120212 with GSK2126458 enhances cell growth inhibition and decreases S6 ribosomal protein phosphorylation in drug-resistant clones from the A375 BRAF(V600E) and the YUSIT1 BRAF(V600K) melanoma cell lines[2]. GSK2126458 potentiates the antiproliferative activity of DDR1-IN-1 in colorectal cancer cell lines[3].
      • 体内研究:
      • In a BT474 human tumor xenograft model, GSK2126458 treatment results in a dose-dependent reduction in pAkt-S473 levels, and exhibits dose-dependent tumor growth inhibition at a low dose of 300 μg/kg. Besides, GSK2126458 shows low blood clearance and good oral bioavailability in four preclinical species (mouse, rat, dog, and monkey)[1]. 
      • 简介:
      • GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively. Ki: 0.019 nM (p110α), 0.13 nM (p110β), 0.024 nM (p110δ), 0.06 nM (p110γ), 0.18 nM (mTORC1), 0.3 nM (mTORC2)
      • 特异性:
      • Target: PI3K. Fields: GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively. Ki: 0.019
      • 来源:
      • Rabbit
      • 稀释:
      • Ki: 0.019 nM (p110α), 0.13 nM (p110β), 0.024 nM (p110δ), 0.06 nM (p110γ), 0.18 nM (mTORC1), 0.3 nM (mTORC2)
      • 浓度:
      • >98%
      • 储存:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • 其他名称:
      • GSK212; GSK-2126458; GSK 2126458; GSK-212; GSK 212,GSK458,GSK 458,GSK2126458
      • 分子量:
      • 505.5
      • 产品图片